Chemical Name: EVT302
Therapy Type: Small Molecule (timeline)
Target Type: Other Neurotransmitters (timeline), Other (timeline)
Condition(s): Alzheimer's Disease
U.S. FDA Status: Alzheimer's Disease (Phase 2)
Company: Evotech AG, Roche
RG1577 was developed by Roche but first licensed to Evotech AG, which began developing it as EVT302 for the treatment of nicotine dependence. That development was discontinued in Phase 2 (see Berlin et al., 2012).
Evotech AG claimed on its website that EVT302 was safer and more tolerable than other MAOB inhibitors marketed for the treatment of Parkinson's disease (see company press release). The compound was reported to be more selective for MAOB over MAOA, a related enzyme that helps metabolize tyramine, a component of certain foods and beverages. For a review on MAO inhibitors, see Finberg, 2014.
Roche and Evotech partner in the development of EVT302/RG1577 for Alzheimer's disease, both to reduce oxidative stress in the brain and to treat dopamine-related symptoms in AD. Roche scientists reported that the compound in enzyme assays is 500-fold selective for human MAOB over MAOA, dose-dependently inhibits MAOB in rat brain at low doses, does not elevate blood pressure in the presence of tyramine, and reduces H2O2 production near amyloid deposits in AD brain sections (Borroni et al., 2013).